33 ISSN: 2347-7881 PharmaTutor Magazine | Vol. 2, Issue 12 | magazine.pharmatutor.org Review Article Role of Prodrugs in Solubility Enhancement of Drugs Kalyana Chakravarthi G*, Vijayaraj S, Venugopal A, Naresh Ch, Saritha B Department of Pharmaceutical Analysis, Sree Vidyanikethan College of Pharmacy, Tirupati, Andhra Pradesh, India. kalyanyadav896@gmail.com ABSTRACT Solubility is one of the essential parameters to achieve bioavailability of drug in systemic circulation to produce expected therapeutic response. Nearly 40% of new drug molecules face solubility challenge. Though several techniques like micronization, crystal engineering, hydrotrophy, solid dispersion and so forth were available for solubility enhancement of poorly soluble drugs based on physical and chemical modification, prodrug approach is a vital technique amongst the other. Prodrugs are biologically inactive compound which can be metabolized in the body to produce active drug. It is estimated that currently about 10% of all world-wide approved drugs are prodrugs. This review extensively confers the role of prodrugs and the kind of promoieties used for solubility enhancement. Keywords: Prodrugs, Solubility Enhancement of Drugs, dissolution rate, bioavailability INTRODUCTION The poor solubility and low dissolution rate of poorly water soluble drugs in the aqueous gastrointestinal fluids often cause insufficient bioavailability. The major challenge with the design of oral dosage forms lies with their poor bioavailability. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. As for BCS class-II drugs rate limiting step is drug release from the dosage form and solubility and not the absorption, so increasing the solubility in turn increases the bioavailability for BCS class-II drugs [1] . Prodrug is biologically inactive compound which can be metabolized in the body produce drug. [2] The prodrug approach is emerged tool to overcome the various obstacles in drug formulation and targeting the chemical instability, low aqueous solubility, local irritation and toxicity. [3] Figure No.1. A simplified illustration of the prodrug concept (Kristiina M. Huttunen et al., Pharmrev.aspetjournals.org, 2011) How to cite this article: KG Chakravarthi, S Vijayaraj, A Venugopal, Ch Naresh, B Saritha; Role of Prodrugs in Solubility Enhancement of Drugs; PharmaTutor; 2014; 2(12); 33-48